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Status:
US Approved Rx
(2023)
Source:
ANDA213267
(2023)
Source URL:
First approved in 1998
Source:
NDA020785
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Thalidomide is an immunomodulatory agent with a spectrum of activity that is not fully characterized. Thalidomide is racemic — it contains both left and right-handed isomers in equal amounts: one enantiomer is effective against morning sickness, and the other is teratogenic. The enantiomers are converted to each other in vivo. That is, if a human is given D-thalidomide or L-thalidomide, both isomers can be found in the serum. Hence, administering only one enantiomer will not prevent the teratogenic effect in humans. In patients with erythema nodosum leprosum (ENL) the mechanism of action is not fully understood. Available data from in vitro studies and preliminary clinical trials suggest that the immunologic effects of this compound can vary substantially under different conditions, but may be related to suppression of excessive tumor necrosis factor-alpha (TNF-a) production and down-modulation of selected cell surface adhesion molecules involved in leukocyte migration. For example, administration of thalidomide has been reported to decrease circulating levels of TNF-a in patients with ENL, however, it has also been shown to increase plasma TNF-a levels in HIV-seropositive patients. As a cancer treatment, the drug may act as a VEGF inhibitor. Thalidomide is used for the acute treatment of the cutaneous manifestations of moderate to severe erythema nodosum leprosum (ENL). Also for use as maintenance therapy for prevention and suppression of the cutaneous manifestations of ENL recurrence. Thalidomide is sold under the brand name Immunoprin, among others.
Status:
Investigational
Source:
NCT01929044: Phase 3 Interventional Completed Intestinal Diseases
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Anisodamine is a naturally occurring atropine derivative that has been isolated, synthesized and characterized by scientists in the People's Republic of China. Anisodamine is a non-specific cholinergic antagonist. Anisodamine has been shown to interact with and disrupt liposome structure which may reflect its effects on cellular membranes. Experimental evidence implicates anisodamine as an anti-oxidant that may protect against free radical-induced cellular damage. Its cardiovascular properties include depression of cardiac conduction and the ability to protect against arrhythmia induced by various agents. Anisodamine is a relatively weak alpha(1) adrenergic antagonist which may explain its vasodilating activity. Its anti-thrombotic activity may be a result of inhibition of thromboxane synthesis. Numerous therapeutic uses of anisodamine have been proposed including treatment of septic shock, various circulatory disorders, organophosphorus (OP) poisoning, migraine, gastric ulcers, gastrointestinal colic, acute glomerular nephritis, eclampsia, respiratory diseases, rheumatoid arthritis, obstructive jaundice, opiate addiction, snake bite and radiation damage protection. The primary therapeutic use of anisodamine has been for the treatment of septic shock. Several mechanisms have been proposed to explain its beneficial effect though most mechanisms are based upon the assumption that anisodamine ultimately acts by an improvement of blood flow in the microcirculation. Preliminary studies suggest another important therapeutic use of anisodamine is for the treatment of OP poisoning. Anisodamine has been employed
therapeutically since 1965 in the People’s Republic of China primarily to improve blood flow in circulatory disorders such as septic shock, disseminated intravascular coagulation (DIC) and as an antidote to organophosphate poisoning.
Status:
Investigational
Source:
NCT00002209: Phase 1 Interventional Completed AIDS Dementia Complex
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
CPI-1189 is a synthetic benzamide with antioxidant properties that blocks tumor necrosis factor-alpha (TNFalpha) effects in animal models. It has neuroprotective properties in model systems for HIV-associated neurotoxicity and thus is a candidate for neuroprotective therapy in humans with HIV-associated CNS disease. CPI-1189 was at the phase II stage of clinical development for the treatment of dementia associated with Parkinson's disease and AIDS Dementia Complex, however, development has been discontinued.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Harpagide and harpagoside are two iridoid glycosides existing in many medicinal plants. They are believed to be the main bioactive compounds related to the anti-inflammatory efficacy of these plants. In vitro Harpagide has shown cytotoxic activity against tumor cell lines A431, HeLa and MCF7. Harpagide emerged as a leishmanicidal agent. Harpagide is common in nature and is known to possess anti-inflammatory activity. In addition, it has been shown that the hydrolysed products of harpagoside and harpagide have more pronounced anti-inflammatory activity when compared to the unhydrolysed compounds.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Aucubin is found in common verbena. Aucubin is a monoterpenoid based compound. Aucubin, like all iridoids, has a cyclopentan-[C]-pyran skeleton. Aucubin is found in the leaves of Aucuba japonica (Cornaceae), Eucommia ulmoides (Eucommiaceae), and Plantago asiatic (Plantaginaceae), etc, plants used in traditional Chinese and folk medicine. Aucubin was found to protect against liver damage induced by carbon tetrachloride or alpha-amanitin in mice and rats when 80 mg/kg was dosed intraperitoneally. Aucubin has been shown to exhibit anti-proliferative and apoptotic functions. Aucubin has shown effectiveness as antifungal and suggests its promising potential use as solution for C. albicans biofilm-related infections. Aucubin has a range of biological activities, including anti-inflammatory, anti-microbial, anti-algesic as well as anti-tumor activities.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Asperuloside, an iridoid glycoside found in Herba Paederiae, is a component from traditional Chinese herbal medicine. Asperuloside is extracted from many traditional Chinese medicinal plants, including Herba Paederiae, Asperula odorata, Goldhair Hedyotis Herb and Hedyotis diffusa. It has been proved that there are many kinds of pharmacological effects such as anti-tumor and anti-obesity activities. Asperuloside can significantly downregulate tumor necrosis factor alpha (TNF-α), interleukin (IL)-1β, and IL-6 levels in vitro and in vivo, and treatment with asperuloside significantly reduced the lung wet-to-dry weight, histological alterations and myeloperoxidase activity in a murine model of LPS-induced acute lung injury (ALI). Asperuloside exerts its anti-inflammatory effect in correlation with inhibition of a pro-inflammatory mediator through suppressing nuclear factor kappa-B (NF-κB) nuclear translocation and MAPK phosphorylation. Asperuloside can be a potential treatment for ALI and can be used as a clinical anti-infective drug.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Menthone is a naturally occurring organic compound. It is found in oils of peppermint, Japanese mint, pennyroyal, Micromeria abyssinica benth, geranium and other oils. It is widely used as fragrances and flavors in the cosmetic, perfume, drug, and food industries. Menthone is a naturally occurring pesticide. Menthone and isomenthone were mild skin irritants and of low acute dermal toxicity in rabbits. Neither showed any sensitizing potential in volunteer studies with dilute solutions. In rats, menthone demonstrated a moderate to low acute oral toxicity. On repeated oral administration, menthone produced increases in liver, kidney and spleen weights of rats. Mutagenic activity was reported for menthone in the bacterium Salmonella typhimurium (Ames test) and in fruitflies.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Stigmastanol is a plant lipid molecule that resembles cholesterol in structure. It inhibits cholesterol absorption. Sitostanol powder (1 g) reduced cholesterol absorption by only 11.3 /- 7.4% (P = 0.2), confirming in vitro data showing poor solubility of sitostanol powder in artificial bile. In contrast, sitostanol in lecithin micelles reduced cholesterol absorption by 36.7 /- 4.2% (P = 0.003) at a dose of 700 mg and by 34.4 /- 5.8% (P = 0.01) at a dose of 300 mg. Stigmasterol, which is used for the synthesis of progesterone and vitamin D3 is a potential anti-inflammatory compound. Its action is mediated by the inhibition of several pro-inflammatory and matrix degradation mediators involved in osteoarthritis-induced cartilage degradation.
Status:
Possibly Marketed Outside US
First approved in 1970
Source:
NDA209184
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Dipalmitoylphosphatidylcholine (DPPC) is the main lipid component of surfactant, it reduces surface tension, preventing collapse of the alveoli. It is used in the treatment of neonatal respiratory distress. It is an important constituent of the number of surfactant, such as Curosurf®, Lucinactant, Exosurf.
Porcine-derived lung surfactant Curosurf® (poractant alfa) intratracheal suspension is indicated for the rescue treatment of respiratory distress syndrome (RDS) in premature infants. Each milliliter of suspension contains 80 mg of poractant alfa that includes 76 mg of phospholipids and 1 mg of protein of which 0.45 mg is SP-B and 0.59 mg is SP-C. The amount of phospholipids is calculated from the content of phosphorus and contains 55 mg of phosphatidylcholine of which 30 mg is dipalmitoylphosphatidylcholine. Curosurf reduces mortality and pneumothoraces associated with RDS.
Lucinactant is a new synthetic peptide-containing surfactant for intratracheal use. It contains sinapultide, phospholipids (dipalmitoylphosphatidylcholine, DPPC and palmitoyloleoyl phosphatidylglycerol, POPG) and a fatty acid (palmitic acid). Intended for the prevention of RDS in premature infants at high risk for RDS. FDA approved on March 6, 2012.
Exosurf, approved by FDA in 1990, is a protein-free surfactant composed of 85% dipalmitoylphosphatidylcholine, 9% hexadecanol, and 6% tyloxapol by weight.